The emu (Dromiceius novae-hollandiae) is the second largest member of the group of flightless birds and is indigenous to Australia. Emus can be raised like ordinary farm animals and used for their valuable products, which include very low fat meat, supple leather hides, decorative and nutritional eggs, and rich oil. Emu oil may be extracted or rendered from the body fat of the emu and is known to contain triglyceride esters of long-chain saturated and unsaturated fatty acids, including oleic acid, linoleic acid, palmitic acid, and stearic acid.
Atopic dermatitis and other forms of eczema are inflammatory, pruritic (i.e., itchy) skin diseases that affect between 10 and 20 percent of the United States (U.S.) population, causing considerable morbidity, poor quality of life, and high medical costs for both the patient and society. Topically administered glucocorticoids are a main form of therapy; however, prolonged use of topical glucocorticoids is associated with skin thinning, permanent stretch marks, dermal atrophy, rebound effects, tachyphylaxis, and potential systemic absorption, which can cause numerous systemic side effects. Topical calcineurin inhibitors (e.g., Elidel® and Protopic® creams and ointments) are effective but are infrequently used as a result of FDA-required “black box” warnings concerning a potential increase in systemic malignancies in patients using these topical preparations.
Psoriasis is also a chronic pruritic inflammatory skin disease affecting 2% of the U.S. population. Inflammation and tumor necrosis factor-alpha (“TNF-alpha”) are of crucial importance in the pathogenesis of psoriasis and its treatment. Based on the severity of the disease presentation, topical glucocorticoids, and vitamin D analogs, either by themselves or in combination with phototherapy or systemic agents (such as methotrexate, cyclosporine A, Humira®, Stelara®, Soriatane®, etc.), have been used for therapy. However, these agents can be extremely expensive, costing more than $20,000 per year per patient.
Histamine is a compound involved in local immune responses of humans and other animals. As part of an immune response to foreign pathogens, histamine is produced by basophils and mast cells found in nearby connective tissues. Upon release from these cells, histamines produce increased vascular permeability, causing fluid to escape from capillaries into tissues, which can lead to inflammation and itchiness among other responses. Histamine triggers an immune system response by combining with specific cellular histamine receptors. The four histamine receptors that have been discovered in humans and animals are designated H1 through H4. Compounds, known as antihistamines, have been developed that do not prevent the release of histamine but instead inhibit the action of histamine by blocking it from attaching to the histamine receptors. Most commonly used antihistamines inhibit action specifically at the H1 receptor and are referred to as H1 antihistamines. While some H1 antihistamines have sedative side effects, so-called “second generation” or “non-sedating” antihistamines do not cross the blood-brain barrier and, thus, do not cause drowsiness. Further, not all H1 antihistamines inhibit the inflammatory response that results from the release of histamine in humans.
Zemtsov is credited with discovering and confirming the presence of the phosphocreatine molecule (“Pcr”) in human skin. Pcr has been found in both skin and internal organs, like skeletal muscle, and is an important energy storage molecule. Pcr assists in regenerating adenosine triphosphate (“ATP”) molecules during periods of high metabolic demand, or ischemia. In turn, ATP molecules produce the energy required for all cellular functions. Topical application of Pcr can “recharge” skin cells. However, Pcr is a very unstable molecule. Nonetheless, Pcr can be regenerated by skin cells by topically applying a mixture of creatine and creatinine, denoted as “Cr/Crt.” Topical mixtures of Cr/Crt have been used for the treatment and prevention of wrinkles and similar cosmetic applications. However, Cr/Crt has not previously been used in medical applications.
Extensive investments of time and capital are required to obtain Federal Drug Administration (FDA) approval to sell and market a new drug. The cost of approval is one reason that only three topical dermatological drugs were approved by the FDA in the last five years. Instead, pharmaceutical companies are primarily directing their efforts to develop and patent new delivery systems and formulations to more efficiently carry active ingredients (i.e., drugs) through the stratum corneum skin barrier. These new formulations include solid lipid nanoparticles, liposomes and niosomes, transferosomes, ethosomes, cyclodextrins, and sol-gel microcapsules.
Accordingly, there is a need for an anti-inflammatory, antipruritic, and moisturizing topical formulation for treating and promoting the healing of wounds and inflammatory conditions of the skin.